Endomorphin-1

SKU: orb1218552

Description

Endomorphin 1 is a high affinity and selective agonist of the μ-opioid receptor and displays reasonable affinities for kappa3 binding sites (Ki: 20~30 nM).

Images & Validation

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Key Properties

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CAS Number	189388-22-5
MW	610.67
Purity	>98% (HPLC)
Formula	C₃₄H₃₈N₆O₅
SMILES	C1C[C@H](N(C1)C(=O)[C@H](CC2=CC=C(C=C2)O)N)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC5=CC=CC=C5)C(=O)N
Target	Opioid Receptor
Solubility	Water:24 mg/mL (39.3 mM; Need ultrasonic)

Bioactivity

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In Vivo

Endomorphin 1 (i. c. v.) shows antinociceptive properties in mice, with an ED50 value of 6.16 nM. Endomorphin 1 (50 μg/kg, i. v.) alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response. Animal model: ICR mice. Dosage: 6.16 nM (ED50. Administration: Intracerebroventricularly (i. c. v.) injection. Result: Inhibited dose-dependently the tail-flick response. Animal model: Rats. Dosage: 50 μg/kg. Administration: Intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min. Result: Alleviated MIRI by reducing the production of free radicals. Dncreased LDH and CK-MB activities. Increased SOD activity and decreased MDA content. Decreased IL-6 and TNF-α plasma content.

In Vitro

Endomorphin 1 inhibits Forskolin (HY-15371) (1 μM) stimulated cyclic AMP formation with a pIC50 value of 8.03 in In CHOμ cells. Endomorphin 1 (1-10 μM) increases interleukin-8 secretion in Caco-2 cells. Endomorphin 1 (1 μM) inhibits excitatory transmission in adult rat substantia gelatinosa neurons.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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Gene Symbol

Opioid Receptor

Protocol Information

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Purity:	> 95% by hplc
MW:	610.67 Da
Structure:	H-Tyr-Pro-Trp-Phe-NH2

Purity:	> 95%
MW:	610.72
Source:	Synthetic

Applications:	ICC, IHC
Reactivity:	Human, Mouse, Rat
Species/Host:	Rabbit
Clonality:	Polyclonal
Conjugation:	Unconjugated

Applications:	ICC, IHC
Reactivity:	Human, Mouse, Rat
Species/Host:	Rabbit
Clonality:	Polyclonal
Conjugation:	Unconjugated

Endomorphin-1

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

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